Cyclin-dependent kinase inhibitors for cancer treatment
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Solution Overview
Problem
There is a need for additional cyclin-dependent kinase inhibitors suitable for pharmaceutical use, particularly targeting CDK4, CDK6, and CDK9, which are deregulated in cancer cells due to overexpression or loss of endogenous inhibitors.
Innovation Solution
Development of specific compounds and their pharmaceutically acceptable salts, represented by Formulae I to XX, which act as modulators of cyclin-dependent kinases, inhibiting CDK4, CDK6, and other CDKs to treat cancer and other disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If existing CDK inhibitors are used to target deregulated CDKs in cancer cells, then therapeutic effects are achieved, but additional effective inhibitors are needed to overcome resistance and expand treatment options
Solution Approach 1:
The patent segments the CDK inhibitor development by creating distinct chemical series (Formulae I-XX) with different core structures and substituent patterns, each potentially offering unique binding characteristics and resistance profiles, thereby expanding the arsenal of available therapeutic agents
Solution Approach 2:
The patent systematically varies chemical parameters including substituent types (R1-R5), ring structures (saturated/unsaturated), and molecular configurations to generate diverse inhibitor analogs with potentially differentiated efficacy, selectivity, and pharmacokinetic properties
Data Source
AI summary
Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.